Unit:
Κατεύθυνση Κλινικές Μελέτες: Σχεδιασμός και ΕκτέλεσηLibrary of the School of Health Sciences
Supervisors info:
Μαρία Γαβριατοπούλου, Επίκουρη Καθηγήτρια, Ιατρική σχολή, ΕΚΠΑ
Ευστάθιος Καστρίτης, Αναπληρωτής Καθηγητής, Ιατρική Σχολή, ΕΚΠΑ
Μαγδαληνή Μήγκου, Ιατρός PhD, Ιατρική Σχολή, ΕΚΠΑ
Original Title:
Ο ρόλος των αναστολέων της BTΚ στις αιματολογικές κακοήθειες
Translated title:
The role of BTK inhibitors in hematologic malignancies
Summary:
B-cell malignancies represent a heterogeneous group of hematologic malignancies with different behavioral patterns and responses to treatment, including most non-Hodgkin's lymphomas (NHLs), some leukemias, and myeloma. Some examples are mantle cell lymphoma (MCL), Waldenström macroglobulinemia (WM) and chronic lymphocytic leukemia (CLL). Bruton tyrosine kinase is a key component of B-cell receptor signaling and functions as an important regulator of cell proliferation and survival in B-cell malignancies. The first class BTK inhibitor Ibrutinib is a small molecule drug that is covalently linked to BTK and has been shown to be an effective treatment for various B-cell malignancies. However, it has off-target activities on non-BTK-related kinases that are associated with side effects or may cause clinical limitations, with reference to Ibrutinib resistance as well. Much progress has been made in developing more selective second-generation BTK inhibitors. It is worth noting a recent change in the mechanisms of action of BTK inhibitors and now new inhibitors are being developed that act through non-covalent inhibition of BTK. The aim of this study is to investigate their evolutionary course in the treatment of hematological malignancies, to describe their main characteristics and to summarize the clinical developments of the second generation BTK inhibitors for the treatment of hematological malignancies. Finally, a brief overview of new non-covalent BTK inhibitors is included.
Main subject category:
Health Sciences
Keywords:
BTK Inhibitors, Ibrutinib, Acalabrutinib, Zanubrutinib, Treatment
Number of references:
231
